Cat. No.: HY-N10319

Artepillin C

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Based on 1 Customer Validation

Artepillin C is an orally active CREB/CRTC2 inhibitor and TRPA1 covalent agonist (EC₅₀=1.8 μM). Artepillin C inhibits CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression to regulate glucose and lipid metabolism. Artepillin C can also activate TRPA1 channels to induce spicy taste signals. Artepillin C can inhibit tumor cell proliferation, induce necroptosis, improve insulin resistance and inhibit liver lipid synthesis. Artepillin C can be used in the study of metabolic syndrome, tumor prevention and treatment, and inflammation.

For research use only. We do not sell to patients.

Purity: 99.07%
CAS No.: 72944-19-5
Formula: C₁₉H₂₄O₃
Molecular Weight:300.39

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Artepillin C Chemical Structure

CAS No.: 72944-19-5

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[3]

CREB/CRTC2

TRPA1

1.8 μM ()

All Epigenetic Reader Domain Isoforms :

All TRP Channel Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	25 μM Compound: ARC	Growth inhibition of human A549 cells Growth inhibition of human A549 cells	[PMID: 28814374]
DU-145	IC₅₀	179 μM Compound: 1	Antiproliferative activity against human DU-145 cells assessed as cell viability for 72 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as cell viability for 72 hrs by MTT assay	[PMID: 34454129]
HeLa	IC₅₀	7 μg/mL Compound: 1	Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA	[PMID: 19942440]
HT-1080	ED₅₀	45.47 μg/mL Compound: 5	Cytotoxicity against human HT1080 cells after 24 hrs by MTT assay Cytotoxicity against human HT1080 cells after 24 hrs by MTT assay	[PMID: 9677271]
MCF-10A	CC₅₀	>200 μM Compound: 1	Cytotoxicity against human MCF-10A cells assessed as cell viability for 72 hrs by MTT assay Cytotoxicity against human MCF-10A cells assessed as cell viability for 72 hrs by MTT assay	[PMID: 34454129]
MCF7	IC₅₀	162.3 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as cell viability for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell viability for 72 hrs by MTT assay	[PMID: 34454129]
MDA-MB-231	IC₅₀	172.7 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability for 72 hrs by MTT assay	[PMID: 34454129]
PC-3	IC₅₀	178.9 μM Compound: 1	Antiproliferative activity against human PC-3 cells assessed as cell viability for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as cell viability for 72 hrs by MTT assay	[PMID: 34454129]
PNT2	CC₅₀	187.6 μM Compound: 1	Cytotoxicity against human PNT2 cells assessed as cell viability for 72 hrs by MTT assay Cytotoxicity against human PNT2 cells assessed as cell viability for 72 hrs by MTT assay	[PMID: 34454129]

In Vitro

Artepillin C (1 μM-1 mM; 12-48 h) inhibits the viability of HEp-2 tumor cells in a concentration- and time-dependent manner, with a CC₅₀ of 4.07 μM-0.9 μM^[1].
Artepillin C (1-0.5 μM; 24 h) induces HEp-2 cell necrosis and significantly increases cell membrane permeability^[1].
Artepillin C (1 μM; 30 min; pH 3.2) enhances the membrane permeability of DPPS-containing macropinosomes (GUVs) and significantly accelerates the efflux of fluorescent probes^[1].
Artepillin C (3.13-50 μg/mL; 36 h) inhibits HUVEC cell tube formation in a concentration-dependent manner, and completely inhibits it at 50 μg/mL^[2].
Artepillin C (3.13-50 μg/mL; 3 d) inhibits HUVEC cell proliferation with an IC₅₀ of approximately 37.2 μg/mL^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[1]

Cell Line:

HEp-2 cells
Concentration:

0.01 mM, 0.05 mM, 0.1 mM, 0.5 mM
Incubation Time:

24 h
Result:

Increased propidium iodide (PI)-positive cells, indicating membrane permeabilization and necrosis.
Morphological changes included cell swelling and granular nuclei, characteristic of necrotic cell death, without significant apoptosis induction.

In Vivo

Artepillin C (0.125%-0.5% diet; po; once a day; 6 days) inhibits tumor-induced angiogenesis in the mouse dorsal air sac tumor model and reduces the number of blood vessels in a dose-dependent manner^[2].
Artepillin C (20 mg/kg; intraperitoneal injection; once a day; 1-3 weeks) significantly improves glucose homeostasis, reduces fasting blood glucose and insulin resistance, inhibits hepatic BMAL1 expression and lipid synthesis-related genes, and reduces hepatic lipid accumulation in db/db obese mice^[4].
Artepillin C (20 mg/kg; intraperitoneal injection; once a day; 3 weeks) improves insulin sensitivity, reduces hepatic gluconeogenesis and lipid synthesis, and regulates the expression of the circadian rhythm-related gene Bmal1 in DIO mice fed a high-fat diet^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

ICR mice (female, 30±5 g, 7-week-old), dorsal air sac (DAS) tumor angiogenesis model^[2]
Dosage:

0.125%, 0.25%, 0.5% (w/w in diet)
Administration:

Oral administration via diet, once daily, 6 days starting from chamber implantation
Result:

Significantly reduced tumor-induced angiogenesis in a dose-dependent manner.
No signs of toxicity were observed, with stable body weight throughout the treatment period.
Histological analysis confirmed reduced vascular density in the treated groups, indicating anti-angiogenic activity without systemic toxicity.

Chemical Information

CAS No. 72944-19-5
Appearance Solid
Molecular Weight 300.39
Formula C₁₉H₂₄O₃
Color Light yellow to yellow
SMILES

C/C(C)=C\CC1=C(C(C/C=C(C)\C)=CC(/C=C/C(O)=O)=C1)O
Structure Classification
- Ketones, Aldehydes, Acids
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (332.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3290 mL

16.6450 mL

33.2901 mL

5 mM

0.6658 mL

3.3290 mL

6.6580 mL

10 mM

0.3329 mL

1.6645 mL

3.3290 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Kobal MB,et al. Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranes. Mater Sci Eng C Mater Biol Appl. 2020 Jul;112:110943. [Content Brief]

[2]. Ahn MR, et al. Suppression of tumor-induced angiogenesis by Brazilian propolis: major component artepillin C inhibits in vitro tube formation and endothelial cell proliferation. Cancer Lett. 2007 Jul 18;252(2):235-43. [Content Brief]

[3]. Hata T, et al. Artepillin C, a major ingredient of Brazilian propolis, induces a pungent taste by activating TRPA1 channels. PLoS One. 2012;7(11):e48072. [Content Brief]

[4]. Wang L, et al. Artepillin C Time-Dependently Alleviates Metabolic Syndrome in Obese Mice by Regulating CREB/CRTC2-BMAL1 Signaling. Nutrients. 2023 Mar 28;15(7):1644. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.3290 mL	16.6450 mL	33.2901 mL	83.2251 mL
	5 mM	0.6658 mL	3.3290 mL	6.6580 mL	16.6450 mL
	10 mM	0.3329 mL	1.6645 mL	3.3290 mL	8.3225 mL
	15 mM	0.2219 mL	1.1097 mL	2.2193 mL	5.5483 mL
	20 mM	0.1665 mL	0.8323 mL	1.6645 mL	4.1613 mL
	25 mM	0.1332 mL	0.6658 mL	1.3316 mL	3.3290 mL
	30 mM	0.1110 mL	0.5548 mL	1.1097 mL	2.7742 mL
	40 mM	0.0832 mL	0.4161 mL	0.8323 mL	2.0806 mL
	50 mM	0.0666 mL	0.3329 mL	0.6658 mL	1.6645 mL
	60 mM	0.0555 mL	0.2774 mL	0.5548 mL	1.3871 mL
	80 mM	0.0416 mL	0.2081 mL	0.4161 mL	1.0403 mL
	100 mM	0.0333 mL	0.1665 mL	0.3329 mL	0.8323 mL

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Artepillin C

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All Epigenetic Reader Domain Isoforms

All TRP Channel Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Artepillin C Related Classifications

HY-N10319 Related Classifications